A series of N-substitutited 11-azaartemisinins were synthesized and several members were found to be four to fives times more active in vitro against drug resistant strains of malaria than the lead compound artemisinin, 1. An in vivo study of the 2'ethanal derivative confirmed the in vitro results. In an effort to increase further the activity of this series an SAR study was undertaken. For this purpose a new synthetic route from 11-azaartemisinin was devised and employed to prepare approximately a dozen additional compounds which contained polar groups on the 3'-carbon. The most active derivative in latter series was also four to five times more active in vitro than 1. Additional attempts to prepare more active derivatives are in progress.In addition, a program utilizing an N-substituted 11-azaartemisinin for the preparation of an affinity chromatographic column has been initiated. The column will be employed to identiy proteins from P. falciparum which bind or react with artemisinin derivatives. Our review on "Artemisinin: An Endoperoxidic Antimalarial from Artemisia annua L." appeared in "Progress in the Chemistry of Organic Natural Products" published by Springer-Verlag in 1997.